C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/56 (2006.01) A61K 38/00 (2006.01) C07K 14/685 (2006.01)
Patent
CA 2609951
Novel backbone cyclized peptides which are a-melanocortin stimulating hormone (aMSH) analogs, having improved Melanocortin-4 receptor agonist activity are disclosed. The backbone cyclized peptide analogs disclosed possess unique and superior properties over other analogs, such as metabolic stability, increased oral bioavailability, improved intestinal permeability and pharmacological activity in-vivo. Pharmaceutical compositions comprising the backbone cyclized aMSH analogs, and methods of using such compositions for the treatment of metabolic disorders including obesity are also disclosed.
L'invention concerne de nouveaux peptides à squelette cyclisé qui sont des analogues de l'hormone .alpha. stimulant la mélanocortine (.alpha.MSH), présentant une activité agoniste du récepteur 4 de la mélanocortine. Ces analogues peptidiques à squelette cyclisé possèdent des propriétés inédites et supérieures à celles d'autres analogues, notamment une stabilité métabolique, une biodisponibilité améliorée par voie orale, une perméabilité intestinale et une activité pharmacologique in vivo accrues. L'invention concerne en outre des compositions pharmaceutiques contenant ces analogues de aMSH à squelette cyclisé, et des méthodes d'utilisation de ces compositions pour le traitement des troubles métaboliques, notamment de l'obésité.
Gilon Chaim
Hess Shmuel
Hoffman Amnon
Linde Yaniv
Ridout & Maybee Llp
Yissum Research Development Company Of The Hebrew University Of
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